Bayer Aktiengesellschaft

Hans-Georg Dellweg

Erwin Bischoff

Elisabeth Perzborn

Ulrich E Muller

Ulrich Niewohner

Johannes-Peter Stasch

Andreas Knorr

Peter Fey

Klaus Frobel

Jan-Bernd Lenfers

Martin Beuck

Ulrich Rosentreter

Hartmund Wollweber

Siegfried Zaiss

Peter Norman

Nigel J Cuthbert

Maarten De Jonge

Hartwig Muller

Hilary P Francis

Bruno Rosen

Wolfgang Piepersberg

Werner Schroder

Jurgen Georg Lenz

Ansgar Stratmann

Jurgen Distler

Anneliese Crueger

Beate Schaper

Klaus Goeke

Hermann Pape

Michael Hemker

The invention relates to acarviosyl transferase from actinomycetes, mainly from Actinoplanes sp. SE 50/110 and its mutants, to a process for isolating, purifying and characterizing the enzyme, to the isolation and characterization of the acbD gene encoding the acarviosyl transferase, to the expression of the acarviosyl transferase in a heterologous host organism, to the use of the acarviosyl transferase for converting acarbose minor constituents into acarbose or for preparing acarbose homologues, to the use of the acarviosyl transferase in acarbose purification, and also to the preparation of production mutants in which formation of minor constituents is reduced by means of inactivation of the acarviosyl transferase gene.

Processes for preparing acarviosyl transferase and for using it in the

N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be prepared either by reaction of aldehydes with acetoacetic esters and amines, optionally with isolation of the corresponding ylidene compounds, or by reaction of aminocrotonic acid esters with ylidene compounds and subsequent alkylation of the NH function. The N-alkylated 1,4-dihydropyridinedicarboxylic acid esters can be employed as active compounds in medicaments, in particular as cerebral therapeutics.

N-alkylated 1,4-dihydropyridinedicarboxylic acid esters

Heterocyclically substituted cycloalkano[b]-indolesulphonamides can be prepared by reaction of appropriate N-unsubstituted indoles with acrylonitrile, followed by hydrolysis, esterification or amidation, or by reaction of heterocyclically substituted hydrazines with cycloalkanones or by subsequent introduction of the heterocyclic group into appropriate indole derivatives. The heterocyclically substituted cycloalkano[b]-indolesulphonamides can be employed for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, asthma, allergies and for the prophylaxis of myocardial infarcts.

Heterocyclically substituted cycloalkano[b]-indolesulphonamides

New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and

Cycloalkano(b)dihydroindoles and -indolesulphonamides substituted by

The invention relates to substituted dibenz-oxa-thiocinone-12-oxides and -12,12-dioxides of the general formula I ##STR1## in which R.sup.1 to R.sup.6 and Y have the meaning indicated in the description, to processes for their preparation and to their use in medicaments, in particular in circulation-influencing medicaments.

Substituted dibenz-oxa-thiocinones, -12-oxides and -12,12-dioxides, a

The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reacton of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkencarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.

Phenylsulphonamide substituted pyridinealkene- and

The compounds according to the invention can be prepared by reaction of the corresponding amines with sulphonic acid derivatives, or in the case of the aminooxy compounds by reaction of ketones with aminooxy compounds or alkylation of hydroxylamines, or in the case of the alkene compounds by reaction of ketones with phosphorusylides. The phenylsulphonamide substituted pyridinealkene- and -aminooxyalkenecarboxylic acid derivatives can be used for the treatment of thromboembolic disorders, ischaemias, arteriosclerosis, allergies and asthma.

Cardioactive compounds of the formula ##STR1## in which R.sup.1 and R.sup.8 and R.sup.14 and R.sup.15 can be hydrogen or various organic radicals.

Circulation-active dibenzo[1,5]dioxocin-5-ones

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Wuppertal, Germany

Hans-Georg Dellweg